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DGK

DGK

Diacylglycerol Kinase (DGK) regulates the equilibrium between phosphatidic acid (PA) and DAG. DAG is phorylated by DGK to produce PA. Ten mammalian DGK subtypes (-) that can be divided into five different types exist. Each subtype has its own tissue distribution. Among them, the production of DAG as a second messenger following stimulation of the T cell receptor is specifically regulated by DGK and DGK. However, in T cells, DGK is the predominant isoform. Certain DGK isoforms that are dysregulated cause DAG-activated PKC, attenuated insulin signaling, and dysregulated glucose metabolism. DGK participates in a variety of physiological processes, such as cell migration and proliferation, glucose uptake, immunity, and the development of neuronal networks.

DGK related products

Structure Cat No. Product Name CAS No. Product Description
(1R)-BMS-986408 V114696 (1R)-BMS-986408 2618418-11-2 (1R)-BMS-986408 is an orally effective dual DGK α/ζ inhibitor.
(5Z,2E)-CU-3 V32186 (5Z,2E)-CU-3 1815598-71-0 (5Z,2E)-CU-3is a novel, potent and selective diacylglycerol kinase alpha (DGKalpha) inhibitorwithanIC50valueof0.6 μM, attenuating cancer cell proliferation and simultaneously enhancing immune responses including anti-cancer immunity.
AHL-7160 V109979 AHL-7160 AHL-7160 is a covalent DGKα inhibitor with dual functions: inhibiting enzyme activity (IC₅₀ ≈ 12 nM) and molecular glue-mediated degradation.
Alcudacigib TFA V113321 Alcudacigib TFA Alcudacigib (compound 9) TFA is a DGKz inhibitor.
AMB639752 V73996 AMB639752 371210-26-3 AMB639752 is a potent DGKα inhibitor.
BAY 2965501 V73987 BAY 2965501 2732902-08-6 BAY 2965501 is a potent and specific diacylglycerol kinase zeta (DGKζ) inhibitor.
BAY-2965501 V51059 BAY-2965501 DGKzeta inhibitor
BMS-332 V74001 BMS-332 2407892-15-1 BMS-332 is a dual (bifunctional) inhibitor of DGKα/ζ lipokinase with IC50 of 0.005 μM (DGKα) and 0.001 μM (DGKζ) respectively.
BMS-496 V73995 BMS-496 2407854-31-1 BMS-496 is a dual (bifunctional) inhibitor of DGKα/ζ lipokinase with IC50 of 0.09 μM (DGKα) and 0.006 μM (DGKζ) respectively.
BMS-502 V73988 BMS-502 2407854-18-4 BMS-502 (Compound 22) is a potent dual (bifunctional) inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50s of 4.6 nM and 2.1 nM.
BMS-684 V73997 BMS-684 313552-29-3 BMS-684 is a selective DGKα inhibitor (antagonist) with IC50 of 15 nM.
BMS-986408 V99706 BMS-986408 2618418-12-3 BMS-986408 is an oral dual DGK α/ζ inhibitor that restores T cell-mediated anti-tumor immunity by enhancing T cell signaling.
Cochlioquinone A (Luteoleersin) V73999 Cochlioquinone A (Luteoleersin) 32450-25-2 Cochlioquinone A is an ATP-competitive diacylglycerol kinase inhibitor (Ki= 3.1 μM).
DGK-IN-1 V73989 DGK-IN-1 2407892-34-4 DGK-IN-1 is a T cell activator from patent WO2020006018A1, Example 25.
DGK-IN-11 V116972 DGK-IN-11 3023735-36-3 DGK-IN-11 (compound 1) is a diacylglycerol kinase (DGK) inhibitor.
DGK-IN-12 V117173 DGK-IN-12 3023735-35-2 DGK-IN-12 is a DGK inhibitor that can be used in cancer research.
DGK-IN-13 V117149 DGK-IN-13 3023735-55-6 DGK-IN-13 is a DGK inhibitor that can be used in cancer research.
DGK-IN-8 V104007 DGK-IN-8 3039488-69-9 DGK-IN-8 (Example 34) is a DGK inhibitor with IC50 ≤ 20 nM for DGKα and ζ.
DGKα&ζ-IN-1 V74000 DGKα&ζ-IN-1 2830643-06-4 DGKα&ζ-IN-1 (Compound II) is a DGK target inhibitor.
DGKα&ζ-IN-2 V117459 DGKα&ζ-IN-2 3039488-61-1 DGKα/ζ-IN-2 is a highly effective, orally active, and selective DGKα/ζ inhibitor with IC50 values of 23 nM (DGKα) and 1.2 nM (DGKζ).
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